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RI-2

现货
Catalog No.
B5881
RAD51抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,800.00
现货
10mg
¥ 4,000.00
现货
50mg
¥ 12,000.00
现货

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Background

Description:

IC50: 44.17 μM

Homologous recombination (HR) is an essential process in cells that provides repair of DNA double-strand breaks and lesions that block DNA replication. RAD51 is an evolutionarily conserved protein that is central to HR. Overexpression of RAD51 protein is common in cancer cells and represents a potential therapeutic target in oncology. RI-2 is an optimized reversible RAD51 inhibitor.

In vitro: Although RI-2 did exhibit reduced activity relative to RI-1, it did retain enough activity to sensitize cells to MMC cell-based assays. RI-2 exhibited no reactivity toward glutathione after incubation for 24 hours. RAD51 protein that had been treated with RI-2 prior to washing exhibited no measurable loss of DNA binding activity, even though RI-2 is known to inhibit RAD51 with an IC50 of 44.17 μM. This indicates that RAD51 inhibition by RI-2 is fully reversible [1].

In vivo: RI-1, the analogue of RI-2, facilitated mapping of the binding pocket within known crystal structures of RAD51. However, this reactivity of RI-1 potentially may limit its development in pre-clinical animal models. RI-1 has been found to exhibit a relatively short half-life, due to reactivity in thiol-containing solutions [1].

Clinical trial: Up to now, RI-2 is still in the preclinical development stage.

Reference:
[1] Budke B, Kalin JH, Pawlowski M, Zelivianskaia AS, Wu M, Kozikowski AP, Connell PP.  An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013 Jan 10;56(1):254-63.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt433.28
Cas No.1417162-36-7
FormulaC21H18Cl2N2O4
Solubility≥21.65mg/mL in DMSO
Chemical Name1-(3,4-dichlorophenyl)-3-(4-methoxyphenyl)-4-morpholino-1H-pyrrole-2,5-dione
SDFDownload SDF
Canonical SMILESCOC1=CC=C(C(C(N2C3=CC(Cl)=C(Cl)C=C3)=O)=C(N4CCOCC4)C2=O)C=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

RI-2